Solubilized Flavonoid Composition via Thermal Processing

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Solution Overview

Problem

Flavonoids, particularly those with planar ring structures like apigenin, exhibit poor solubility in water and most solvents, limiting their bioavailability and effectiveness in pharmaceutical, nutraceutical, and cosmetic applications due to their low solubility, which hinders their absorption and efficacy in treating skin conditions and other diseases.

Innovation Solution

A method involving heating flavonoids with a heat-stable solubilizing compound, such as polysorbate surfactants, to a temperature above 100°C in the absence of a carrier, allowing the flavonoids to dissolve in the surfactant, and then cooling the mixture to maintain solubility at ambient temperatures, thereby increasing their concentration and bioavailability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If flavonoids are used in pharmaceutical and nutraceutical formulations, then therapeutic efficacy is improved, but solubility in water and suitable solvents deteriorates

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidsolubility
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The patent uses heat-stable solubilizing compounds as intermediary substances to bridge the incompatibility between flavonoids and water-based formulations. These solubilizing compounds form soluble complexes with the hydrophobic flavonoid molecules, enabling their incorporation into aqueous pharmaceutical and nutraceutical formulations while maintaining therapeutic efficacy.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent applies temperature parameter changes by heating the formulation to elevated temperatures during the solubilization process. This thermal treatment enhances the solubility of flavonoids in the heat-stable solubilizing compounds, allowing for higher concentrations to be achieved and then maintained upon cooling, thereby improving both solubility and therapeutic efficacy.

Inventive Principle:
Principle #35Parameter changes

2Quantity of substance

If heat treatment is applied to enhance solubility of flavonoids, then solubility is improved, but risk of decomposition deteriorates

Engineering Contradiction:
ImprovesolubilityVSAvoidstability
Core Design Contradiction:
Quantity of substanceVSReliability

Solution Approach 1:

The patent carefully controls the temperature parameter within a specific range (50°C to 100°C) that is sufficient to enhance flavonoid solubility in heat-stable solubilizing compounds but below the decomposition temperature of the flavonoids. This optimized parameter selection allows solubility improvement while preventing thermal degradation.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs heat-stable solubilizing compounds that can withstand the required temperature treatment without degrading. These solubilizing agents act as protective vehicles that tolerate the thermal processing needed for solubility enhancement while protecting the thermally sensitive flavonoid active ingredients from decomposition.

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

This method significantly enhances the solubility and bioavailability of poorly soluble flavonoids, enabling their effective delivery and absorption, thereby improving their therapeutic efficacy in treating skin conditions and other diseases.

Implementation Method 1

heating flavonoids with a heat-stable solubilizing compound, such as polysorbate surfactants, to a temperature above 100°C

Methodology Applied
Scientific EffectHeating: Heating

Implementation Method 2

cooling the mixture to maintain solubility at ambient temperatures

Methodology Applied
Scientific EffectCooling: Cooling

Data Source

PatentEP3345594B1Solubilized flavonoid composition
Publication Date: 2021.11.17 TECH INVESTMENTS LC
  • EP3345594B1 patent drawingFigure 1
  • EP3345594B1 patent drawingFigure 2
  • EP3345594B1 patent drawingFigure 3

AI summary

The subject invention relates to novel soluble forms of planar ring structured organic compounds including flavonoids, and their production. The invention also includes the use of these novel formulations of planar ring structured organic compounds in the preparation of formulations and products. The invention also relates to a wide variety of applications of the formulations of the invention. The subject invention includes novel soluble forms and various formulations of flavonoids. Further, the invention includes novel methods of manufacturing the flavonoid formulations. The invention also relates to a wide variety of applications of the flavonoid formulations.